EP2698375A3 - Modulateurs de TGR5 et leur procédé d'utilisation - Google Patents
Modulateurs de TGR5 et leur procédé d'utilisation Download PDFInfo
- Publication number
- EP2698375A3 EP2698375A3 EP13192394.8A EP13192394A EP2698375A3 EP 2698375 A3 EP2698375 A3 EP 2698375A3 EP 13192394 A EP13192394 A EP 13192394A EP 2698375 A3 EP2698375 A3 EP 2698375A3
- Authority
- EP
- European Patent Office
- Prior art keywords
- disease
- compounds
- tgr5 modulators
- formula
- tgr5
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-n-(4-chlorophenyl)-n,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 title abstract 2
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 title abstract 2
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000020446 Cardiac disease Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 208000008839 Kidney Neoplasms Diseases 0.000 abstract 1
- 206010038389 Renal cancer Diseases 0.000 abstract 1
- 208000010643 digestive system disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000016097 disease of metabolism Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000018685 gastrointestinal system disease Diseases 0.000 abstract 1
- 208000019622 heart disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 201000010982 kidney cancer Diseases 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SI200931820T SI2698375T1 (sl) | 2008-11-19 | 2009-11-19 | Modulatorji TGR5 in njihova uporaba |
NO13192394A NO2698375T3 (fr) | 2008-11-19 | 2009-11-19 | |
EP13192394.8A EP2698375B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de TGR5 et leur procédé d'utilisation |
PL13192394T PL2698375T3 (pl) | 2008-11-19 | 2009-11-19 | Modulatory TGR5 i sposób ich zastosowania |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08169462 | 2008-11-19 | ||
EP09760057.1A EP2376519B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de tgr5 et leur procédé d'utilisation |
EP13192394.8A EP2698375B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de TGR5 et leur procédé d'utilisation |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP09760057.1A Division EP2376519B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de tgr5 et leur procédé d'utilisation |
Publications (3)
Publication Number | Publication Date |
---|---|
EP2698375A2 EP2698375A2 (fr) | 2014-02-19 |
EP2698375A3 true EP2698375A3 (fr) | 2014-03-12 |
EP2698375B1 EP2698375B1 (fr) | 2018-02-21 |
Family
ID=41668454
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP09760057.1A Active EP2376519B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de tgr5 et leur procédé d'utilisation |
EP13192394.8A Active EP2698375B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de TGR5 et leur procédé d'utilisation |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP09760057.1A Active EP2376519B1 (fr) | 2008-11-19 | 2009-11-19 | Modulateurs de tgr5 et leur procédé d'utilisation |
Country Status (23)
Country | Link |
---|---|
US (5) | US8114862B2 (fr) |
EP (2) | EP2376519B1 (fr) |
JP (5) | JP5535233B2 (fr) |
KR (2) | KR101789960B1 (fr) |
CN (2) | CN104370990A (fr) |
AU (1) | AU2009316566B9 (fr) |
BR (1) | BRPI0921983B8 (fr) |
CA (1) | CA2744189C (fr) |
DK (2) | DK2376519T3 (fr) |
EA (2) | EA030681B1 (fr) |
ES (2) | ES2458168T3 (fr) |
HK (2) | HK1166327A1 (fr) |
HU (1) | HUE039171T2 (fr) |
IL (3) | IL212969A (fr) |
LT (1) | LT2698375T (fr) |
MX (1) | MX2011005295A (fr) |
NO (1) | NO2698375T3 (fr) |
PL (2) | PL2376519T3 (fr) |
PT (2) | PT2376519E (fr) |
SG (1) | SG10201400162QA (fr) |
SI (1) | SI2698375T1 (fr) |
WO (1) | WO2010059853A1 (fr) |
ZA (1) | ZA201104077B (fr) |
Families Citing this family (47)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE303399T1 (de) | 2001-03-12 | 2005-09-15 | Intercept Pharmaceuticals Inc | Steroide als agonisten für fxr |
ES2533993T3 (es) | 2004-03-12 | 2015-04-16 | Intercept Pharmaceuticals, Inc. | Tratamiento de fibrosis usando ligandos de FXR |
US10987362B2 (en) | 2004-03-12 | 2021-04-27 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using FXR ligands |
ITMI20050912A1 (it) | 2005-05-19 | 2006-11-20 | Erregierre Spa | Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici |
EP2112995B1 (fr) | 2007-01-19 | 2013-07-31 | Intercept Pharmaceuticals, Inc. | Acides biliares substitues en 23 utiles comme modulateurs de tgr5 et leurs methodes d'utilisation |
CN102164940B (zh) | 2008-07-30 | 2015-08-19 | 英特塞普特医药品公司 | Tgr5调节剂及其使用方法 |
PT2376519E (pt) * | 2008-11-19 | 2014-02-20 | Intercept Pharmaceuticals Inc | Moduladores de tgr5 e métodos da sua utilização |
CN102316872B (zh) | 2008-11-26 | 2016-12-21 | 萨蒂奥根制药公司 | 治疗肥胖症和糖尿病的胆汁酸再循环抑制剂 |
EP2364161B1 (fr) | 2008-11-26 | 2020-03-11 | Satiogen Pharmaceuticals, Inc. | Compositions contenant des satiogènes et leurs procédés d'utilisation |
ES2552657T3 (es) | 2010-05-26 | 2015-12-01 | Satiogen Pharmaceuticals, Inc. | Inhibidores del reciclado de ácidos biliares y saciógenos para el tratamiento de diabetes, obesidad, y afecciones gastrointestinales inflamatorias |
SG10201407013QA (en) | 2011-10-28 | 2014-12-30 | Lumena Pharmaceuticals Inc | Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases |
US9982008B2 (en) | 2012-06-19 | 2018-05-29 | Intercept Pharmaceuticals, Inc. | Preparation and uses of obeticholic acid |
US9238673B2 (en) | 2012-06-19 | 2016-01-19 | Intercept Pharmaceuticals, Inc. | Preparation and uses of obeticholic acid |
EP2906197A1 (fr) | 2012-10-09 | 2015-08-19 | The Procter & Gamble Company | Procédé d'identification de combinaisons cosmétiques synergiques |
EP2906946A1 (fr) | 2012-10-09 | 2015-08-19 | The Procter & Gamble Company | Procédé d'identification ou d'évaluation de principes actifs bénéfiques, et compositions contenant ces derniers |
EP3004132A4 (fr) * | 2013-06-06 | 2017-01-18 | Yissum, Research Development Company of the Hebrew | Conjugués acides biliaires-acides aminés basiques et leurs utilisations |
US20160151486A1 (en) * | 2013-06-13 | 2016-06-02 | Fast Foward Pharmaceuticals B.V. | CD40 Signalling Inhibitor and a Further Compound, Wherein the Further Compound is a Bile Acid, a Bile Acid Derivative, an TGR5-Receptor Agonist, an FXR Agonist or a Combination Thereof, for the Treatment of Chronic Inflammation, and the Prevention of Gastrointestinal Cancer or Fibrosis |
JP6621409B2 (ja) | 2013-11-22 | 2019-12-18 | ミナ セラピューティクス リミテッド | C/EBPα小分子活性化RNA組成物 |
PL3626725T3 (pl) | 2014-05-29 | 2023-04-03 | Bar Pharmaceuticals S.R.L. | Pochodne cholanu do zastosowania w leczeniu i/lub zapobieganiu chorobom, w których pośredniczy fxr i tgr5/gpbar1 |
US20180236064A1 (en) * | 2014-10-03 | 2018-08-23 | Mayo Foundation For Medical Education And Research | Targeting tgr5 to treat disease |
WO2016073767A1 (fr) * | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Analogues d'acide biliaire d'agonistes de fxr/tgr5 et leurs procédés d'utilisation |
CA2968309A1 (fr) | 2014-11-19 | 2016-05-26 | NZP UK Limited | Steroides 6-alkyl-7-hydroxy-4-en-3-one utilises en tant qu'intermediaires pour la production de modulateurs de fxr steroidiens |
TWI686400B (zh) | 2014-11-19 | 2020-03-01 | 英商Nzp英國有限公司 | 化合物(二) |
EA034739B1 (ru) | 2014-11-19 | 2020-03-16 | ЭнЗедПи ЮКей ЛИМИТЕД | 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
CN107207558B (zh) | 2014-11-19 | 2019-10-29 | Nzp英国有限公司 | 作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇 |
CN105985396A (zh) * | 2015-02-16 | 2016-10-05 | 苏州泽璟生物制药有限公司 | 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物 |
JP2018519246A (ja) * | 2015-04-28 | 2018-07-19 | ジエンス ハンセン ファーマセウティカル グループ カンパニー リミテッド | コール酸誘導体、及びその製造方法及び医薬用途 |
DK3310801T3 (da) | 2015-06-19 | 2021-06-21 | Intercept Pharmaceuticals Inc | Tgr5-modulatorer og fremgangsmåder til anvendelse deraf |
WO2016205475A2 (fr) * | 2015-06-19 | 2016-12-22 | Intercept Pharmaceuticals, Inc. | Modulateurs de tgr5 et leurs procédés d'utilisation |
US11072631B2 (en) * | 2015-09-24 | 2021-07-27 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
CR20180201A (es) * | 2015-10-07 | 2018-08-24 | Intercept Pharmaceuticals Inc | Modularores del receptor x farnesoide |
CN106008639B (zh) * | 2016-03-11 | 2019-01-08 | 深圳市塔吉瑞生物医药有限公司 | 用于预防或治疗fxr-介导疾病的胆烷酸化合物 |
JP6968821B2 (ja) | 2016-04-13 | 2021-11-17 | インターセプト ファーマシューティカルズ, インコーポレイテッド | 癌を治療する方法 |
GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
US10654834B2 (en) * | 2016-07-01 | 2020-05-19 | Venenum Biodesign, LLC | Non-systemic TGR5 agonists |
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